Lasamide Containing Sulfonylpiperazines as Effective Agents for the Management of Glaucoma Associated Symptoms DOI Creative Commons
Fabrizio Carta, Jaydeo T. Kilbile, Suryakant B. Sapkal

et al.

ChemMedChem, Journal Year: 2024, Volume and Issue: unknown

Published: Sept. 25, 2024

Abstract A series of 2,4‐dichloro‐5‐{[4‐(phenylsulfonyl)piperazin‐1‐yl]carbonyl}benzenesulfonamides were designed and synthesized through amidation Lasamide 1 with substituted piperazines. The newly obtained compounds demonstrated remarkable inhibition potency selectivity for the human (h) expressed Carbonic Anhydrase (CA; EC 4.2.1.1) II isoform. Selected 7 9 investigated in an vivo model glaucoma showed relevant performances, latter being able to last effect up 4 hours. results herein reported are sustainment derivatives as a new class potentially exploitable management uncontrolled intra ocular pressure (IOP).

Language: Английский

-Derivatization of Natural Tropolone and β-Thujaplicin Leading to effective Inhibitors of Human Carbonic Anhydrases IX and XII DOI Creative Commons
Francesco Melfi, Ilaria D’Agostino, Simone Carradori

et al.

European Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 117552 - 117552

Published: March 1, 2025

Language: Английский

Citations

0
Lasamide Containing Sulfonylpiperazines as Effective Agents for the Management of Glaucoma Associated Symptoms DOI Creative Commons
Fabrizio Carta, Jaydeo T. Kilbile, Suryakant B. Sapkal

et al.

ChemMedChem, Journal Year: 2024, Volume and Issue: unknown

Published: Sept. 25, 2024

Abstract A series of 2,4‐dichloro‐5‐{[4‐(phenylsulfonyl)piperazin‐1‐yl]carbonyl}benzenesulfonamides were designed and synthesized through amidation Lasamide 1 with substituted piperazines. The newly obtained compounds demonstrated remarkable inhibition potency selectivity for the human (h) expressed Carbonic Anhydrase (CA; EC 4.2.1.1) II isoform. Selected 7 9 investigated in an vivo model glaucoma showed relevant performances, latter being able to last effect up 4 hours. results herein reported are sustainment derivatives as a new class potentially exploitable management uncontrolled intra ocular pressure (IOP).

Language: Английский

Citations

0